[CAS NO. 848695-25-0] BIIB021

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PRODUCTS SPECIFICATIONS [848695-25-0]

Catalog

HY-10212

Brand

MCE

CAS

848695-25-0

DESCRIPTION [848695-25-0]

Overview

MDL	MFCD15528939
Molecular Weight	318.76
Molecular Formula	C14H15ClN6O
SMILES	ClC1=C2C(N(C=N2)CC3=C(C(OC)=C(C=N3)C)C)=NC(N)=N1

For research use only. We do not sell to patients.

2 Publications Citing Use of MCE

Summary

BIIB021 (CNF2024) is an orally active, fully synthetic inhibitor of HSP90 with a K _i and an EC ₅₀ of 1.7 nM and 38 nM, respectively ^[1] .

IC50 & Target

HSP90

1.7 nM (Ki)

HSP90

38 nM (EC ₅₀ )

In Vitro

BIIB021 binds in the ATP-binding pocket of Hsp90, interferes with Hsp90 chaperone function, and results in client protein degradation and tumor growth inhibition. BIIB021 inhibits tumor cell (BT474, MCF-7, N87, HT29, H1650, H1299, H69 and H82) proliferation with IC ₅₀ from 0.06-0.31 μM. BIIB021 induces the degradation of Hsp90 client proteins including HER-2, Akt, and Raf-1 and up-regulated expression of the heat shock proteins Hsp70 and Hsp27 ^[1] .
BIIB021 inhibits Hodgkin's lymphoma cells (KM-H2, L428, L540, L540cy, L591, L1236 and DEV) with IC ₅₀ from 0.24-0.8 μM. BIIB021 shows low activity in lymphocytes from healthy individuals. BIIB021 inhibits the constitutive activity of NF-κB despite defective IκB. BIIB021 induces the expression of ligands for the activating NK cell receptor NKG2D on Hodgkin's lymphoma cells resulting in an increased susceptibility to NK cell-mediated killing ^[2] .
BIIB021 enhances the in vitro radiosensitivity of HNSCCA cell lines (UM11B and JHU12) with a corresponding reduction in the expression of key radioresponsive proteins, increases apoptotic cells and enhances G2 arrest ^[3] .
BIIB021 is considerably more active than 17-AAG against adrenocortical carcinoma H295R. The cytotoxic activity of BIIB021 is not influenced by loss of NQO1 or Bcl-2 overexpression, molecular lesions that do not prevent client loss but are nonetheless associated with reduced cell killing by 17-AAG. BIIB021 is also active in 17-AAG resistant cell lines (NIH-H69, MES SA Dx5, NCI-ADR-RES, Nalm6) ^[4] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Oral administration of BIIB021 leads to tumor growth inhibition in many tumor xenograft models including N87, BT474, CWR22, U87, SKOV3 and Panc-1 ^[1] .
BIIB021 effectively inhibits growth of L540cy tumor at a dose of 120 mg/kg ^[2] . BIIB021 significantly enhances antitumor growth effect of radiation in JHU12 xenograft ^[3] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01017198	Biogen	Advanced Solid Tumors	November 2009	Phase 1
NCT00344786	Biogen	B-Cell Chronic Lymphocytic Leukemia	February 2006	Phase 1
NCT00618319	Biogen	GIST	February 2008	Phase 2
NCT00345189	Biogen	Tumors\|Lymphoma	February 2006	Phase 1
NCT00618735	Biogen	Advanced Solid Tumors	February 2008	Phase 1
NCT00412412	Biogen	Breast Cancer	December 2007	Phase 1
NCT01004081	Biogen	Breast Cancer	November 2009	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 45 mg/mL ( 141.17 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.1372 mL	15.6858 mL	31.3716 mL
5 mM	0.6274 mL	3.1372 mL	6.2743 mL
10 mM	0.3137 mL	1.5686 mL	3.1372 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (7.84 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (7.84 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

9H-Purin-2-amine, 6-chloro-9-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]-

6-Chloro-9-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]-9H-purin-2-amine

[6-Chloro-9-(4-methoxy-3,5-dimethylpyridin-2-ylmethyl)-9H-purin-2-yl]amine

BIIB 021

CNF 2024